Kinase Chemistry – Just a year and a half behind the times.

Rational design…

Posted by kinasepro on November 5, 2008

? ~ F(x) has some thoughts.

Ever since Captopril, I’ve always thought ‘rational design’ to be over-rated and over-sold.  We can do an awful lot without pin-point accuracy, and frankly we don’t have to understand why something is safe and effective to make it so.  Perhaps Ashutosh has tickled a nerve by bringing it up, but I fail to understand why people prefer this fanciful delusion of rational design to the reality of knowledge-based trial and error, but the primary literature is chock full-o-nuts claiming to be a lot smarter then they really are.  But I digress…

On non-oncology indications, of course Fasudil was approved in Japan in 1995 for ‘vascular spasms in the brain’ or some suchness, and is in Ph3 in the US for a few indicationsPfizer and Incyte each have related Jak inhibitors which have looked promising in Ph2 studies.  Otherwise your looking at Rigel’s Ph2 Syk / Flt3 / Vegf inhibitor R-788 also in trials for RA but more likely to be approved for more acute indications, and then there’s always the p38 inhibitors, like Array’s recent ph2, but who knows if and when this target will deliver.

The fact that there was a Kinase-related conference and nobody could rattle that off suggests I’m not posting enough…


One Response to “Rational design…”

  1. Ashutosh said

    Clearly you are not posting enough! Or maybe it was just the 7:30 a.m. time.
    Drug discovery is always going to be a combination of ‘rational’ and ‘irrational’ approaches; your point that rationality is overrated is as well taken there as it is in geopolitical strategy. My project did involve at least some targeted thinking, so I can vouch for at least a marginal role for rationality there.
    Thanks for the plug and the links.

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